• Archives of Pharmacal Research
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• 제28권5호
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• pp.509-517
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• 2005

A series of structurally diverse amide derivatives of [6-(3,5-dimethyl-4- chloro-pyrazole-1-yl)-3(2H)-pyridazinone-2-yl]acetic acid were prepared and tested for their in vivo analgesic and anti-inflammatory activity by using p-benzoquinone-induced writhing test and carrageenan induced hind paw edema model, respectively. The analgesic and anti-inflammatory activity of the compounds, 7c, 7d and 7k were found to be equipotent to aspirin (as an analygesic) and indometacin (as an anti-inflammatory drug), respectively. The other amide derivatives generally resulted in lower activity on comparision with reference compounds.

• Bulletin of the Korean Chemical Society
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• 제34권8호
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• pp.2480-2486
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• 2013

A new series of diarylamides and diarylureas having 2,3-dihydropyrrolo[3,2-b]quinoline scaffold was synthesized. Their in vitro antiproliferative activities were tested over NCI-60 cancer cell lines of nine different cancer types. Some target compounds showed good inhibition percentages over different cell lines. Among all the target compounds, compound 1f possessing 6,7-dimethoxy-2,3-dihydropyrrolo[3,2-b]quinoline nucleus, amide linker, and 4-chloro-3-(trifluoromethyl)phenyl terminal ring showed high selectivity against MCF7 and MDA-MB-468 breast cancer cell lines more than the other tested cell lines. Its inhibition percentages at $10{\mu}M$ concentration over those two cell lines were 84.97% and 87.13%, respectively.

• Bulletin of the Korean Chemical Society
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• 제28권10호
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• pp.1641-1642
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• 2007

• Archives of Pharmacal Research
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• 제14권1호
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• pp.48-51
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• 1991

Amides from amino acid ester and nalidixic acid were synthesized. The solubility characteristics and partition coefficient of the compounds were studied. The hydrolysis of the compounds was studied in the simulated gastric fluid and simulated intestinal fluid. Some compounds showed better antibacterial activity than nalidixic acid.

• 한국응용과학기술학회지
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• 제35권1호
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• pp.173-185
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• 2018

화학 관능기가 다른 지방산 에스터계, 지방산 금속염 및 아마이드계 분산 및 흐름개선 첨가제가 EPDM과 카본블랙을 충전제로 사용한 고무 배합물의 가류 특성과 가류된 고무 배합물의 기계적 물성 및 노화특성에 미치는 영향을 무니점도계, 레오미터, 경도계, 만능재료시험기 등을 이용하여 측정하였다. $125^{\circ}C$에서 측정된 무니점도는 아마이드계 > 금속염계 > 에스터계 첨가제의 순으로 감소하는 경향을 보였으며, 스코치시간은 에스터계와 금속염계 첨가제는 첨가 유무에 따라 거의 차이가 없거나 조금 늦어지며, 아마이드계 첨가제는 1분 이상 빨라졌다. $160^{\circ}C$에서의 레오미터 측정 결과 가류시간은 금속염계와 아마이드계 첨가제의 경우는 가류반응이 빨리 진행되었다. 델타토크 값은 금속염계와 아마이드계 첨가제가 있는 경우 전반적으로 증가하였으나, 에스터계 첨가제가 있는 경우는 약간 감소하였다. EPDM 배합물의 인장강도는 에스터계 첨가제가 첨가된 경우 크게 향상되었으며, 아마이드계와 금속염계 첨가제의 경우는 큰 영향이 없었다. 신율의 경우는 금속염계 첨가제의 경우 크게 향상되었으며, 나머지의 경우는 큰 영향이 없었다. 인열강도는 첨가제의 첨가에 따라 전반적으로 상승하였으며 금속염계 첨가제의 경우에서 확연히 상승하였으며 경도는 첨가제의 종류와 상관없이 유사한 값을 나타내었다. $100^{\circ}C$에서 24시간 열노화시킨 EPDM 배합물은 금속염계와 아마이드계 첨가제의 경우는 거의 변화가 없었으며 신율의 변화는 첨가제를 함유한 모든 EPDM 배합물이 10-20% 정도 감소하는 경향을 보였다.

• Bulletin of the Korean Chemical Society
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• 제27권9호
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• pp.1353-1358
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• 2006

We investigated in vitro T-cell inhibitory activity and bioavailability of small chemical inhibitors for Lck SH2 domain, which had a different scaffold such as an amide bond, reduced amide bond, N-methyl amide bond, thioamide bond, and urethane bond. Each of these compounds, with its particular scaffold, showed a different logP value, stability against serum enzyme, stability in buffer solution, and in vitro T-cell inhibitory activity. Overall results indicated that the SH2 inhibitor containing urethane bond can be a new lead compound because of its superior bioavailability, potent in vitro T-cell inhibitory activity, and facile synthesis.

• Bulletin of the Korean Chemical Society
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• 제32권3호
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• pp.1022-1026
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• 2011

The syntheses of DTPA-bis(amide) conjugates of phosphonated cyclohexane moieties (5a-d) and their Gd(III) complexes of the type $[Gd(L)(H_2O)]{\cdot}nH_2O$ (6a-d; L = 5a-d) are described. All new compounds have been characterized by microanalysis and spectroscopic techniques. High $r_1$ relaxivities of aqueous solutions of 6a-d are observed to be in the range of $10.7-18.3\;mM^{-1}sec^{-1}$, which compare much better than that of $Omniscan^{(R)}$ ($r_1=3.90\;mM^{-1}sec^{-1}$).

• Korean Membrane Journal
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• 제3권1호
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• pp.9-16
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• 2001

The diamide-diamine having carboxylic acid was prepared by direct condensation of 1,2,4-benzenetricarboxylic acid with bits[4- (3-aminophenoxy ) phenyl] sulfone and bits(4-aminouhenyl)-1,4- diisopropylbenzene in medium consisting of triphenylphosphite, LiCl, and N-methyl-2-pyrrolidone. Copoly (amide-imide) derivatives with high molecular weight could be synthesized by one-step polycondensation of prepared diamide-diamine having carboxylic acid and various dianhydride compounds. Depending on the chemical structure and composition of polymer backbones, the viscosities of polymers were found to range between 0.87∼ 1.57 dL/B. All the polymers showed good thermal stability up to 320$\^{C}$ and the 10% weight loss temperature was observed in the range of 450∼540$\^{C}$ in a thermogravimetric traces. The glass transition was recorded in the temperature range of 200 ∼ 270$\^{C}$. All the polymers showed an amorphous nature on a differential scanning calorimetric thermograms. These polymers generally had good mechanical properties and readily soluble in various polar solvents. Further, it was proved that their properties could be determined from the composition.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.186.1-186.1
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• 2003

Bradykinin is an autocoid related to acute and chronic pain and inflammation. The non-peptide bradykinin antagonists are of interest as novel anti-inflammatory therapeutics. Some active compounds such as FR 173657, LF 160687, and bradyzide were reported very recently. In our search for the new bradykinin antagonists, we designed and synthesized the iminodiacetic acid derivatives having two or three amide bonds and lipophilic ring system in each molecule. Liquid phase combinatorial synthesis using the iminodiacetic acid template gave diverse individual compounds rapidly and efficiently on a 10-50 mg scale. (omitted)

• Bulletin of the Korean Chemical Society
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• 제32권7호
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• pp.2497-2500
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• 2011